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Inhibition of Hepatitis C Virus Envelop Protein E2 Binding To Its Cellular Receptor, CD81 by Imidazole-4-5-Dicarboxamide Derivatives

Reference Number: 01-30

Inventors: Scott Todd and Paul Baures


Current therapy for Hepatitis C virus (HCV) infection involves the use of general immune modulator, a-interferon, in combination with ribavirin. There therapy has limited efficacy. New small molecule therapeutics for the treatment of HCV infection are needed. The interaction of human CD81 (the cellular receptor for HCV-E2) protein and the HCV envelope protein (E2) is believed to be important in the infectivity of HCV. Additionally, binding of HCV-E2 to CD81 on T cells alters the T cell function which may enable HCV to manipulate or evade immune response and persist in the patient for many years.

Highlights of the Invention
  • Several small molecules synthesized at Kansas State University have been found to block binding of HCV-E2 to CD81 on human cell lines
  • These novel molecules may act as peptidomimetics of CD81 to disrupt interactions between HCV-E2 and CD81, thereby inhibiting binding of the virus to the cellular receptor
  • The best inhibitor to date has an approximate IC 50 value 45mM in the in vitro assay
  • It is expected that further variation of this structure will improve its affinity and solubility characteristics
  • The scaffolds used for the development of the compounds are relatively simple to prepare, have predictable conformations and are amphiphilic in order to aid solubility in both water and cell membranes
  • An additional application of the invention is the use of these scaffolds as a general proteomimetic scaffold for studying other protein-protein interactions
Patent Status
  • U.S. Patent #7,208,628 issued on Aril 24, 2007

Kansas State University Research Foundation seeks to have discussions with companies that are interested in licensing and/or research collaborations.

Interested parties should contact:

Kansas State University Institute for Commercialization (KSU-IC)
2005 Research Park Circle Manhattan, KS 66502
Tel: 785-532-3900 Fax: 785-532-3909
E-Mail: ic@k-state.edu